Drug – bio-affecting and body treating compositions – Plant material or plant extract of undetermined constitution... – Containing or obtained from vitis
Reexamination Certificate
2000-05-23
2001-07-24
Prats, Francisco (Department: 1651)
Drug, bio-affecting and body treating compositions
Plant material or plant extract of undetermined constitution...
Containing or obtained from vitis
C424S725000, C424S757000, C426S655000
Reexamination Certificate
active
06264997
ABSTRACT:
BACKGROUND OF THE INVENTION
The present invention relates to an anti-arteriosclerotic food containing a proanthocyanidin and an isoflavone.
Cardiovascular diseases attributed to arteriosclerosis, such as ischemic cardiopathy and cerebral infarct, have given rise to a serious social problem on account of their high death rates in Europe and America. Japan has also been suffering a steep increase of cardiovascular diseases caused by arteriosclerosis with westernization of diet. For the time being, drug treatment of the arteriosclerotic cardiovascular diseases has a limit, and prevention by food-derived components, especially antioxidant substances is considered important. Various antioxidants of food origin, for example vitamin C and vitamin E have been studied to date from the standpoint of prevention of arteriosclerosis but have not yet attained sufficient prophylactic effects.
Prevention of arteriosclerosis by flavonoids has been attracting attention and been under study. In particular, proanthocyanidins were found to have an inhibitory effect on arteriosclerosis equally to probucol, an antihyperlipemic. However, since there is a limit of absorption of proanthocyanidins from the intestinal canal, the effects obtained from proanthocyanidins, even if ingested in a large quantity, are limited (see Jun Yamakoshi, et al., Atherosclerosis, vol. 142, pp. 139-149 (1999)). Isoflavones, on the other hand, exhibit dose-dependent effects when ingested alone but fail to produce a sufficient effect unless taken in a large amount.
SUMMARY OF THE INVENTION
An object of the present invention is to provide an anti-arteriosclerotic food which is more effective at a smaller amount than known anti-arteriosclerotic foods.
As a result of extensive studies, the present inventor has found that a combined se of a proanthocyanidin and an isoflavone as active ingredients produces synergism thereby to provide anti-arteriosclerotic foods which are more effective even when taken in a small amount and completed the present invention. The mechanism of the synergism is believed to reside in that oxidation of LDL (low density lipoprotein) which takes an important role in developing arteriosclerosis is suppressed by proanthocyanidin's capturing active oxygen species outside LDL and isoflavone's capturing active oxygen species inside and outside LDL.
DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS
Proanthocyanidins are condensed tannin present in various plant parts, i.e., a group of condensation or polymerization compounds comprising, as a constituent unit, flavan-3-ol or flavane-3,4-diol. These compounds release anthocyanidins, such as cyanidin, delphinidin, and pelargonidin, upon being treated with an acid, on which the above naming is based. Proanthocyanidins include procyanidin, prodelphinidin, propelargonidin, and the like which may be oligomers made up of two, three or four units or polymers made up of ten or more units; and stereoisomers thereof. They are obtained by extracting various plant parts, such as grape seeds, cranberry fruit, apple fruit, adzuki beans (red beans), and bark of sugi trees (Japanese cedar), hinoki trees (Japanese cypress) or pine trees.
Products comprising proanthocyanidins as a main ingredient are available on the market, including Gravinol and KPA (both available from Kikkoman Corp.; prepared from grape seeds), Applephenon (available from The Nikka Whisky Distilling Co., Ltd.; prepared from immature apple fruit), and Pycnogenol (available from Horphag Research Ltd., Switzerland; prepared from bark of maritime pine trees).
The isoflavones which can be used in the present invention are obtained from various plant parts and roughly divided into glycosides and aglycons (non-sugar moieties of glycosides). Many of naturally-occurring isoflavones are glycosides. Isoflavone glycosides ingested into the body are decomposed by &bgr;-glycosidase to release aglycons, which are ready to be absorbed. Some persons are unable to take in aglycons because of lack of &bgr;-glycosidase. Therefore, isoflavone aglycons are superior to isoflavone glycosides in bioavailability.
Specific examples of isoflavones are daidzin, glycitin, genistin, daidzein, glycitein, genistein, 6″—O-acetyldaizin, 6″—O-malonyldaizin, 6″—O-acetylglycitin, 6″—O-malonylglycitin, 6″—O-acetylgenistin, and 6″—O-malonylgenistin. These isoflavones can be obtained by extracting various plant parts, such as leguminous plants (e.g., soybean and red clover (Trifolium pratense)), composite plants, and iridaceous plants. Isoflavones are also extractable from by-products obtained in the manufacture of tofu (soybean curd), miso (soybean paste), soy sauce, isolated soybean protein, and the like, such as liquid used for boiling soybeans and soybean whey. The extracted isoflavone glycosides may be treated with &bgr;-glycosidase or microorganisms having &bgr;-glycosidase to obtain the corresponding aglycons. Isofavones are also obtained by extracting soy sauce cake which is characterized by its high content of isoflavone aglycons.
Products comprising isoflavones as main ingredients are commercially available, including SoyAct (isoflavone aglycons prepared from fermented soybean extract; available from Kikkoman Corp.), Novasoy (isoflavone glycosides prepared from soybeans, available from ADM Comp.), and Promensil (isoflavone aglycons prepared from red clover, available from Novogen Inc.).
It is essential for the anti-arteriosclerotic food according to the present invention to contain both a proanthocyanidin and an isoflavone as active ingredients. If desired, these essential active ingredients can be mixed with appropriate auxiliary components such as vehicles and made into convenient forms such as powders, tablets and capsules ready to be taken as health foods, nutrient subsidiary foods, or specified heath foods. Further, the food of the present invention can be added to various beverages and foods to make healthy foods. The food of the present invention can further contain various food ingredients, food additives or drugs which are inhibitory on arteriosclerosis, such as vitamin C and vitamin E.
Effective intakes of the proanthocyanidin and the isoflavone (in terms of aglycon) of the anti-arteriosclerotic food are 10 mg or more, preferably 20 to 500 mg, and 5 mg or more, preferably 10 to 300 mg, respectively, per day for an adult weighing, for example, 60 kg.
REFERENCES:
patent: 4232122 (1980-11-01), Zilliken
patent: 5904924 (1999-05-01), Gaynor
patent: 5997935 (1999-12-01), Diamond
Yamakoshi, J. et al. Proanthocyanidin-rich extract from grape seeds attenuates the dvelopment of aoritc atherosclerosis in cholesterol- fed rabbiots, Atherosclerosis, p. 139-149 of vol. 142, 1999.*
E. A. Kirk et al., “Dietary Isoflavones Reduce Plasma Cholesterol and Atherosclerosis in C57BL/6 Mice but not LDL Receptor-Deficient Mice,” 1998 American Society for Nutritional Sciences, pp. 954-959.
Izumi Toru
Obata Akio
Saito Makoto
Tobe Koichiro
Yamakoshi Jun
Kikkoman Corporation
Prats Francisco
Srivastava K. C.
Young & Thompson
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